Process for producing...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/32 (2006.01)

Patent

CA 2616117

It is intended to provide a process for producing 1-benzyl-4-[(5,6-dimethoxy-1- indanone)-2-ylidene]methylpiperidine represented by the structural formula (I): (I) which is useful as an intermediate material for a pharmaceutical or a solvate thereof in which impurity content is further reduced and operation is simple and suitable for industrial production by reacting 5,6-dimethoxy-1- indanone with 1-benzyl-4-formylpiperidine in a reaction solvent in the presence of a base and then gradually crystallizing a target substance in a reaction mixture in a high temperature region.

L'invention a pour objet un procédé servant à produire de la 1-benzyl-4-[(5,6-diméthoxy-1-indanone)-2-ylidène]méthylpipéridine représentée par la formule de structure (I) : (I) laquelle est utile comme intermédiaire pour un produit pharmaceutique ou un solvate de celui-ci et a une teneur en impuretés encore réduite, lequel procédé est simple à mettre en oeuvre, convient pour une production à l'échelle industrielle et comprend de faire réagir du 5,6-diméthoxy-1-indanone avec de la 1-benzyl-4-formylpipéridine dans un solvant de réaction en présence d'une base et de faire ensuite cristalliser progressivement la substance cible dans le mélange de réaction dans une zone à haute température.

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